Antiprotozoal activity of synthetic amino substituted 1-methyl-1 H-alpha-carbolines
Verbeeck, S.; Yadav, A.K.; Maes, B.U.W.; Augustyns, K.; Van Der Veken, P.; Cos, P.; Maes, L.; Pieters, L.
Die Pharmazie 69(2): 83-85
2014
ISSN/ISBN: 0031-7144 PMID: 24640594 Document Number: 674610
The antiprotozoal properties of a series of amino substituted 1-methyl-1 H-alpha-carbolines were investigated in a broad panel of parasites. Various substituents were systematically introduced at various positions on the carbocyclic ring of the parent 1-methyl-1 H-alpha-carboline. Most compounds showed a potent antiprotozoal activity, although mostly accompanied by cytotoxicity on MRC-5 cells. One compound, containing the same amino-substitution as chloroquine, showed an IC50 against Plasmodium falciparum of 2.37 microM and was reasonably selective.